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Assay Detail

CHEMBL3762038

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant c-Met (unknown origin) using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hepatocyte growth factor receptor (CHEMBL3717)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.
Liu Y, Jin S, Peng X, Lu D, Zeng L, Sun Y, Ai J, Geng M, Hu Y.
Eur J Med Chem (2016) 108 : 322 -333
PubMed 26698536 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.95 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL601719 CRIZOTINIB 4.0 1 8.85
CHEMBL3758464 1 8.44
CHEMBL3759495 1 8.37
CHEMBL3758452 1 8.37
CHEMBL3759100 1 8.25
CHEMBL3758564 1 8.14
CHEMBL3759079 1 8.12
CHEMBL3759336 1 8.09
CHEMBL3758926 1 7.98
CHEMBL3760077 1 7.91
CHEMBL3759611 1 7.87
CHEMBL3758865 1 7.80
CHEMBL3758752 1 7.80
CHEMBL3758905 1 7.73
CHEMBL3758780 1 7.70
CHEMBL3759319 1 7.67
CHEMBL3758647 1 7.55
CHEMBL3759229 1 7.27
CHEMBL3759320 1 7.09
CHEMBL3758597 1 -
CHEMBL3758362 1 -
CHEMBL3758256 1 -
CHEMBL3758539 1 -
CHEMBL3758418 1 -
CHEMBL3758187 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL601719 CRIZOTINIB IC50 = 1.4 nM 8.85
CHEMBL3758464 IC50 = 3.6 nM 8.44
CHEMBL3759495 IC50 = 4.3 nM 8.37
CHEMBL3758452 IC50 = 4.3 nM 8.37
CHEMBL3759100 IC50 = 5.6 nM 8.25
CHEMBL3758564 IC50 = 7.3 nM 8.14
CHEMBL3759079 IC50 = 7.5 nM 8.12
CHEMBL3759336 IC50 = 8.1 nM 8.09
CHEMBL3758926 IC50 = 10.5 nM 7.98
CHEMBL3760077 IC50 = 12.2 nM 7.91
CHEMBL3759611 IC50 = 13.6 nM 7.87
CHEMBL3758865 IC50 = 15.9 nM 7.80
CHEMBL3758752 IC50 = 15.9 nM 7.80
CHEMBL3758905 IC50 = 18.8 nM 7.73
CHEMBL3758780 IC50 = 20.1 nM 7.70
CHEMBL3759319 IC50 = 21.2 nM 7.67
CHEMBL3758647 IC50 = 27.9 nM 7.55
CHEMBL3759229 IC50 = 53.2 nM 7.27
CHEMBL3759320 IC50 = 82.1 nM 7.09
CHEMBL3758597 IC50 > 100.0 nM -
CHEMBL3758362 IC50 > 100.0 nM -
CHEMBL3758256 IC50 > 100.0 nM -
CHEMBL3758539 IC50 > 100.0 nM -
CHEMBL3758418 IC50 > 100.0 nM -
CHEMBL3758187 IC50 > 100.0 nM -